[Lys(DOTA)(4)]BVD15, a novel and potent neuropeptide Y analog designed for Y(1) receptor-targeted breast tumor imaging.
Bioorganic & medicinal chemistry letters 2009 Dec 23; In press
Guérin B, Dumulon-Perreault V, Tremblay M MC, Ait-Mohand S, Fournier P, Dubuc C, Authier S, Bénard F
Centre d'imagerie moléculaire de Sherbrooke (CIMS), Department of Nuclear Medicine and Radiobiology, Université de Sherbrooke, 3001, 12th North Avenue Sherbrooke, Québec, Canada J1H 5N4.
We substituted a truncated neuropeptide Y (NPY) analog, [Pro(30), Tyr(32), Leu(34)]NPY(28-36)NH(2) also called BVD15, at various positions with DOTA (1,4,7,10-tetraazacyclododecane-1,4,7-10-tetraacetic acid) and evaluated the effect of the coupling position with the binding affinity for NPY Y(1) receptors (NPY1R). Our data suggest that [Lys(DOTA)(4)]BVD15 (K(i)=63+/-25nM vs. K(i)=39+/-34nM for BVD15) is a potent NPY analog suitable for radiolabeling with metallo positron emitters for PET imaging of breast cancer.
Keywords: neuropeptide Y breast tumor imaging breast cancer
